Sunday
2:00 pm - 9:00 pm
Arrival and Check-in
6:00 pm - 7:00 pm
Dinner
7:30 pm - 7:40 pm
Introductory Comments by GRC Staff / Welcome and Introduction from the Chairs
7:40 pm - 9:30 pm
7:40 pm - 8:05 pm
"Inhaled Administration for Intra-Cellular Targets Exemplified by the Discovery of FRAP1 (mTOR kinase) Inhibitors"
8:05 pm - 8:20 pm
Discussion
8:20 pm - 8:45 pm
"Discovery of NVP-MIW491: Dermal Delivery of an LXR Agonist for the Treatment of Meibomian Gland Dysfunction"
8:45 pm - 8:55 pm
Discussion
8:55 pm - 9:20 pm
"Development of a Colon-Targeted Pan-SIK Inhibitor for the Treatment of IBD"
9:20 pm - 9:30 pm
Discussion
Monday
7:30 am - 8:30 am
Breakfast
9:00 am - 12:30 pm
New Frontiers in Oncology Therapies
9:00 am - 9:30 am
"IL4I1 Inhibitors from Target Validation Through to First-In-Human Studies in Cancer Patients"
9:30 am - 9:45 am
Discussion
9:45 am - 10:15 am
"Identification of Dencatistat: An Isoform Selective CTPS1 Inhibitor for Multiple Oncology Indications"
10:15 am - 10:30 am
Discussion
10:30 am - 11:00 am
Coffee Break
11:00 am - 11:30 am
"Structure- and Property-Based Design of Macrocyclic pan-KRAS Inhibitors"
11:30 am - 11:45 am
Discussion
11:45 am - 12:15 pm
"Discovery of MOMA-341, a Chemically Distinct, Potent and Selective Covalent Inhibitor of Werner Syndrome Helicase (WRN)"
12:15 pm - 12:30 pm
Discussion
12:30 pm - 1:30 pm
Lunch
1:30 pm - 4:00 pm
Free Time
4:00 pm - 6:00 pm
Poster Session
6:00 pm - 7:00 pm
Dinner
7:30 pm - 9:30 pm
Deconvolution Strategies for Phenotypic Screens
7:30 pm - 8:00 pm
"Discovery and Optimization of the First Specific Ribosome Biogenesis Inhibitor Targeting the AAA-ATPase NVL"
8:00 pm - 8:10 pm
Discussion
8:10 pm - 8:40 pm
"Phenotypic Screening and Target Deconvolution: Identification of a Chemical Series with Antiviral Activity Against Sarbecovirus with a Novel Mechanism of Action"
8:40 pm - 8:50 pm
Discussion
8:50 pm - 9:20 pm
"Identification of HbF-Activating CELMoDs™ Through Phenotypic Screening and the Subsequent Development of the ZBTB7A/WIZ Dual Degrader BMS-986470 for the Treatment of Sickle Cell Disease"
9:20 pm - 9:30 pm
Discussion
Tuesday
7:30 am - 8:30 am
Breakfast
9:00 am - 12:30 pm
Innovations in Medicinal Chemistry to Advance Peptide Therapeutics
9:00 am - 9:30 am
"Oral Peptide Inhibitors of IL-1β for ASCVD"
9:30 am - 9:45 am
Discussion
9:45 am - 10:15 am
"Orally Bioavailable Macrocyclic Peptide Cyclin A/B RxL Inhibitors to Treat Cancers with High E2F Activity"
10:15 am - 10:30 am
Discussion
10:30 am - 11:00 am
Group Photo / Coffee Break
11:00 am - 11:30 am
"Discovery of FOG-001, a Clinical Stage Helicon Inhibitor of the Beta-Catenin/TCF4 Interaction"
11:30 am - 11:45 am
Discussion
11:45 am - 12:15 pm
"Advances in Peptide Conjugates: Exemplified by Macrocyclic Peptidic Degraders"
12:15 pm - 12:30 pm
Discussion
12:30 pm - 1:30 pm
Lunch
1:30 pm - 4:00 pm
Free Time
4:00 pm - 6:00 pm
Poster Session
6:00 pm - 7:00 pm
Dinner
7:30 pm - 9:30 pm
Overcoming Challenges in Achieving and Measuring Effective Therapeutic Concentration
7:30 pm - 8:00 pm
"Discovery of GS-4182, a Lenacapavir Prodrug to Treat HIV Infection with Once-Weekly Oral Administration"
8:00 pm - 8:10 pm
Discussion
8:10 pm - 8:40 pm
"Rapid Optimization of RUVBL1/2 Inhibitors Enabled by Single-Molecule Tracking"
8:40 pm - 8:50 pm
Discussion
8:50 pm - 9:20 pm
"Discovery of a Clinical Gut-Restricted KEAP1-NRF2 Inhibitor for the Treatment of Inflammatory Bowel Disease"
9:20 pm - 9:30 pm
Discussion
Wednesday
7:30 am - 8:30 am
Breakfast
9:00 am - 12:30 pm
9:00 am - 9:30 am
"Inhibition of Multiple System Atrophy with a New Class of Stacking Ligands for Fibrillar α-Synuclein"
9:30 am - 9:45 am
Discussion
9:45 am - 10:15 am
"Discovery of [11 C]MK-7337, A Novel High-Affinity Alpha-Synuclein PET Ligand for Imaging in Idiopathic Parkinson’s Disease Patients"
10:15 am - 10:30 am
Discussion
10:30 am - 11:00 am
Coffee Break
11:00 am - 11:30 am
"Discovery of Novel Azaindazole GluN2B NAMs"
11:30 am - 11:45 am
Discussion
11:45 am - 12:15 pm
"Discovery of VENT-02: a Highly Brain-Penetrant NLRP3 Inhibitor for the Treatment of Neuroinflammatory Disorders"
12:15 pm - 12:30 pm
Discussion
12:30 pm - 1:30 pm
Lunch
1:30 pm - 4:00 pm
Free Time
4:00 pm - 6:00 pm
Poster Session
6:00 pm - 7:00 pm
Dinner
7:30 pm - 9:30 pm
Use of Artificial Intelligence and Machine Learning in Medicinal Chemistry, Challenges, Opportunities and the Limits
7:30 pm - 8:00 pm
"AI in Drug Discovery: Revolution, Evolution, or Complete Nonsense"
8:00 pm - 8:10 pm
Discussion
8:10 pm - 8:40 pm
"Are Co-Folding Methods Ready for Prime Time?"
8:40 pm - 8:50 pm
Discussion
8:50 pm - 9:20 pm
"Painting a Picture of AI at AstraZeneca: An HPK1 Case Study"
9:20 pm - 9:30 pm
Discussion
Thursday
7:30 am - 8:30 am
Breakfast
8:30 am - 9:00 am
Business Meeting
Nominations for the Next Vice Chair(s); Complete the GRC Evaluation Forms; Election of the Next Vice Chair(s)
9:00 am - 12:30 pm
Late-Breaking Topics: First Disclosures of Clinical Candidates
9:00 am - 9:30 am
"Discovery of a First-in-class Molecular Glue Degrader, BMS-986463, for the Treatment of Advanced Malignant Solid Tumors"
9:30 am - 9:45 am
Discussion
9:45 am - 10:15 am
"Discovery of Clinical Candidate PF-07293893: A Novel and Selective AMPKγ3 Activator for the Treatment of Heart Failure"
10:15 am - 10:30 am
Discussion
10:30 am - 11:00 am
Coffee Break
11:00 am - 11:30 am
"Discovery of GS-1427: A Potent, Selective, Oral Small Molecule Inhibitor of α4β7 for the Treatment of Inflammatory Bowel Disease"
11:30 am - 11:45 am
Discussion
11:45 am - 12:15 pm
"Discovery of MOMA-313, a Potent and Selective Inhibitor of the Polymerase Theta Helicase Domain for the Treatment of HR-Deficient Tumors"
12:15 pm - 12:30 pm
Discussion
12:30 pm - 1:30 pm
Lunch
1:30 pm - 4:00 pm
Free Time
4:00 pm - 6:00 pm
Poster Session
6:00 pm - 7:00 pm
Dinner
7:30 pm - 9:30 pm
Keynote Session: Humanizing Drug Discovery
7:30 pm - 8:30 pm
"Humanizing Drug Discovery"
8:30 pm - 8:55 pm
Discussion
8:55 pm - 9:15 pm
General Discussion
9:15 pm - 9:30 pm
Closing Remarks
Friday
7:30 am - 8:30 am
Breakfast
9:00 am
Departure